一系列新的2-氨基苯并噻唑杂环与噻唑烷-2,4-二酮4a-e、1,3,4-噻二唑芳基脲6a-d和氰基硫脲结构8a-d相连的混合物已经被合成。采用索拉非尼(SOR)作为标准药品，对新的混合物进行了对三种癌细胞系，即HCT-116、HEPG-2和MCF-7的体外抗肿瘤效应进行了评估。在测试的化合物中，4a表现为最有效，其IC50分别为5.61、7.92和3.84微米。此外，化合物4e和8a在乳腺癌细胞株中表现出强烈的影响，其IC50分别为6.11和10.86微米。这三种化合物对正常WI-38细胞显示出良好的安全性。在MCF-7细胞中，三种化合物的流式细胞术分析表明，化合物4a和4c抑制了S期细胞群体，而8a则抑制了G1 / S期细胞群体。最有前途的化合物被用于VEGFR-2抑制试验，其中4a被证明是VEGFR-2的最佳活性抑制剂，其IC50为91微米，而SOR的IC50为53微米。计算机辅助分析显示，这三种新的混合物成功地连接到了像共结晶抑制剂SOR一样的活性位点上。

A new series of 2-aminobenzothiazole hybrids linked to thiazolidine-2,4-dione 4a-e, 1,3,4-thiadiazole aryl urea 6a-d, and cyanothiouracil moieties 8a-d was synthesised. The in vitro antitumor effect of the new hybrids was assessed against three cancer cell lines, namely, HCT-116, HEPG-2, and MCF-7 using Sorafenib (SOR) as a standard drug. Among the tested compounds, 4a was the most potent showing IC50 of 5.61, 7.92, and 3.84 µM, respectively. Furthermore, compounds 4e and 8a proved to have strong impact on breast cancer cell line with IC50 of 6.11 and 10.86 µM, respectively. The three compounds showed a good safety profile towards normal WI-38 cells. Flow cytometric analysis of the three compounds in MCF-7 cells revealed that compounds 4a and 4c inhibited cell population in the S phase, whereas 8a inhibited the population in the G1/S phase. The most promising compounds were subjected to a VEGFR-2 inhibitory assay where 4a emerged as the best active inhibitor of VEGFR-2 with IC50 91 nM, compared to 53 nM for SOR. In silico analysis showed that the three new hybrids succeeded to link to the active site like the co-crystallized inhibitor SOR.